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Zastosuj identyfikator do podlinkowania lub zacytowania tej pozycji: http://hdl.handle.net/20.500.12128/566
Tytuł: Investigation of the biological properties of (hetero)aromatic thiosemicarbazones
Autor: Serda, Maciej
Mrozek-Wilczkiewicz, Anna
Jampilek, Josef
Pesko, Matus
Kralova, Katarina
Vejsova, Marcela
Musioł, Robert
Ratuszna, Alicja
Polański, Jarosław
Słowa kluczowe: Thiosemicarbazones; Iron chelators; In Vitro Anticancer Activity; Lipophilicity; Spinach Chloroplasts
Data wydania: 2012
Źródło: Molecules, (2012), vol. 17, no. 11, p. 13483-13502
Abstrakt: Two series of thiosemicarbazone-based iron chelators (twenty-seven compounds) were designed and synthesized using a microwave-assisted approach. Quinoline and halogenated phenyl were selected as parent scaffolds on the basis of a similarity search. The lipophilicity of the synthesized compounds was measured using HPLC and then calculated. Primary in vitro screening of the synthesized compounds was performed against eight pathogenic fungal strains. Only a few compounds showed moderate activity against fungi, and (E)-2-(quinolin-2-ylvinyl)-N,N-dimethylhydrazine-carbothioamide appeared to be more effective than fluconazole against most of the fungal strains tested. Antiproliferative activity was measured using a human colon cancer cell line (HCT-116). Several of the tested compounds showed submicromolar antiproliferative activity. Compounds were also tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. The structure-activity relationships are discussed for all of the compounds.
URI: http://hdl.handle.net/20.500.12128/566
DOI: 10.3390/molecules171113483
ISSN: 1420-3049
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